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WO2005116653A3 - Recepteur couple a une proteine g humaine et modulateurs associes utilises dans le traitement de l'hyperglycemie et des troubles afferents - Google Patents

Recepteur couple a une proteine g humaine et modulateurs associes utilises dans le traitement de l'hyperglycemie et des troubles afferents Download PDF

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Publication number
WO2005116653A3
WO2005116653A3 PCT/US2005/012447 US2005012447W WO2005116653A3 WO 2005116653 A3 WO2005116653 A3 WO 2005116653A3 US 2005012447 W US2005012447 W US 2005012447W WO 2005116653 A3 WO2005116653 A3 WO 2005116653A3
Authority
WO
WIPO (PCT)
Prior art keywords
modulator
protein
human
gpcr
blood glucose
Prior art date
Application number
PCT/US2005/012447
Other languages
English (en)
Other versions
WO2005116653A2 (fr
Inventor
Jun Qiu
Robert R Webb
David J Unett
Joel E Gatlin
Daniel T Connolly
Original Assignee
Arena Pharm Inc
Jun Qiu
Robert R Webb
David J Unett
Joel E Gatlin
Daniel T Connolly
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Arena Pharm Inc, Jun Qiu, Robert R Webb, David J Unett, Joel E Gatlin, Daniel T Connolly filed Critical Arena Pharm Inc
Priority to JP2007508478A priority Critical patent/JP2007532135A/ja
Priority to AU2005248722A priority patent/AU2005248722A1/en
Priority to US11/578,257 priority patent/US20080306114A1/en
Priority to EP05780020A priority patent/EP1735622A2/fr
Priority to CA002564139A priority patent/CA2564139A1/fr
Publication of WO2005116653A2 publication Critical patent/WO2005116653A2/fr
Publication of WO2005116653A3 publication Critical patent/WO2005116653A3/fr
Priority to US11/604,178 priority patent/US20070231263A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/76—Human chorionic gonadotropin including luteinising hormone, follicle stimulating hormone, thyroid stimulating hormone or their receptors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • General Physics & Mathematics (AREA)
  • Reproductive Health (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)

Abstract

L'invention concerne des procédés qui permettent d'identifier l'existence d'au moins un modulateur d'un récepteur couplé à une protéine G (GPCR) ou d'un modulateur de la glycémie sur un ou plusieurs composés candidats. Dans certains modes de réalisation, le GPCR est humain. Par ailleurs, l'invention concerne des procédés d'utilisation d'un modulateur de GPCR. Un modulateur préféré est un agoniste. Les agonistes de l'invention sont utilisés comme agents thérapeutiques pour faire baisser la glycémie, empêcher ou traiter certains troubles métaboliques, tels que l'insulinorésistance, la diminution de tolérance au glucose, le diabète, ainsi que pour prévenir ou traiter une complication consécutive à une glycémie élevée, telle que l'athérosclérose, la cardiopathie, l'accident vasculaire cérébral, l'hypertension et l'acrosyndrome.
PCT/US2005/012447 2004-04-13 2005-04-12 Recepteur couple a une proteine g humaine et modulateurs associes utilises dans le traitement de l'hyperglycemie et des troubles afferents WO2005116653A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2007508478A JP2007532135A (ja) 2004-04-13 2005-04-12 高血糖症および関連障害の処置のための、ヒトｇタンパク質共役レセプターおよびそのモジュレーター
AU2005248722A AU2005248722A1 (en) 2004-04-13 2005-04-12 Human G protein-coupled receptor and modulators thereof for the treatment of hyperglycemia and related disorders
US11/578,257 US20080306114A1 (en) 2004-04-13 2005-04-12 Human G Protein-Coupled Receptor and Modulators Thereof for the Treatment of Hyperglycemia and Related Disorders
EP05780020A EP1735622A2 (fr) 2004-04-13 2005-04-12 Modulateurs de récepteurs couplés à une protéine g humaine pour le traitement de l'hyperglycémie et de troubles afférents
CA002564139A CA2564139A1 (fr) 2004-04-13 2005-04-12 Recepteur couple a une proteine g humaine et modulateurs associes utilises dans le traitement de l'hyperglycemie et des troubles afferents
US11/604,178 US20070231263A1 (en) 2004-04-13 2006-11-22 Human G protein-coupled receptor and modulators thereof for the treatment of hyperglycemia and related disorders

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56195404P 2004-04-13 2004-04-13
US60/561,954 2004-04-13

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US11/578,257 A-371-Of-International US20080306114A1 (en) 2004-04-13 2005-04-12 Human G Protein-Coupled Receptor and Modulators Thereof for the Treatment of Hyperglycemia and Related Disorders
US11/604,178 Continuation US20070231263A1 (en) 2004-04-13 2006-11-22 Human G protein-coupled receptor and modulators thereof for the treatment of hyperglycemia and related disorders

Publications (2)

Publication Number Publication Date
WO2005116653A2 WO2005116653A2 (fr) 2005-12-08
WO2005116653A3 true WO2005116653A3 (fr) 2006-05-18

Family

ID=35451510

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/012447 WO2005116653A2 (fr) 2004-04-13 2005-04-12 Recepteur couple a une proteine g humaine et modulateurs associes utilises dans le traitement de l'hyperglycemie et des troubles afferents

Country Status (8)

Country Link
US (1) US20080306114A1 (fr)
EP (1) EP1735622A2 (fr)
JP (4) JP2007532135A (fr)
CN (1) CN101027560A (fr)
AU (1) AU2005248722A1 (fr)
CA (1) CA2564139A1 (fr)
TW (1) TW200539867A (fr)
WO (1) WO2005116653A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8921350B2 (en) 2006-12-28 2014-12-30 Cymabay Therapeutics, Inc. Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
US9150567B2 (en) 2009-10-01 2015-10-06 Cymabay Therapeutics, Inc. Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts

Families Citing this family (18)

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CA2537230A1 (fr) 2003-09-05 2005-03-17 Altana Pharma Ag Utilisation d'inhibiteurs de pde4 pour le traitement du diabete sucre
WO2006094942A1 (fr) * 2005-03-08 2006-09-14 Nycomed Gmbh Roflumilast pour le traitement du diabète sucré
EP1874308A1 (fr) 2005-03-08 2008-01-09 Nycomed GmbH Roflumilast pour le traitement de diabetes mellitus
TW200738701A (en) * 2005-07-26 2007-10-16 Du Pont Fungicidal carboxamides
US20070224645A1 (en) * 2006-02-23 2007-09-27 Jianming Lu Novel cell-based phosphodiesterase assays
WO2007115805A2 (fr) * 2006-04-05 2007-10-18 European Molecular Biology Laboratory (Embl) Inhibiteurs de la kinase aurora
US9090604B2 (en) 2006-07-27 2015-07-28 E I Du Pont De Nemours And Company Fungicidal azocyclic amides
WO2008013622A2 (fr) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Amides azocycliques fongicides
ES2531256T3 (es) 2007-01-25 2015-03-12 Du Pont Amidas fungicidas
AU2008279447A1 (en) 2007-07-19 2009-01-29 Metabolex, Inc. N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders
DE102007047735A1 (de) * 2007-10-05 2009-04-09 Merck Patent Gmbh Thiazolderivate
TWI428091B (zh) 2007-10-23 2014-03-01 Du Pont 殺真菌劑混合物
WO2010117090A1 (fr) * 2009-04-10 2010-10-14 Banyu Pharmaceutical Co.,Ltd. Nouveaux dérivés d'isoquinolinyloxyméthyl-hétéroaryle
WO2010117084A1 (fr) * 2009-04-10 2010-10-14 Banyu Pharmaceutical Co.,Ltd. Nouveaux dérivés d'isoquinoline
KR20120101019A (ko) 2009-10-30 2012-09-12 바이엘 크롭사이언스 아게 헤테로아릴피페리딘 및 -피페라진 유도체
CN102753186B (zh) * 2010-01-08 2016-09-14 Isis制药公司 血管生成素样3表达的调节
EP3493807A1 (fr) 2016-08-03 2019-06-12 CymaBay Therapeutics, Inc. Composés d'aryle d'oxyméthylène pour le traitement de maladies gastro-intestinales inflammatoires ou de troubles gastro-intestinaux
CN113082020A (zh) * 2021-04-08 2021-07-09 徐州医科大学 一种腺苷受体激动剂的增强剂及其应用

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EP1378749A1 (fr) * 2001-04-12 2004-01-07 Takeda Chemical Industries, Ltd. Procede de criblage
WO2004058750A1 (fr) * 2002-12-24 2004-07-15 Metris Therapeutics Limited Derives d'acide carboxylique piperidinyl-thiazole servant d'inhibiteurs de l'angiogenese
CA2514547A1 (fr) * 2003-01-28 2004-08-12 Takeda Pharmaceutical Company Limited Agonistes de recepteurs

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WO2004058750A1 (fr) * 2002-12-24 2004-07-15 Metris Therapeutics Limited Derives d'acide carboxylique piperidinyl-thiazole servant d'inhibiteurs de l'angiogenese
CA2514547A1 (fr) * 2003-01-28 2004-08-12 Takeda Pharmaceutical Company Limited Agonistes de recepteurs

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8921350B2 (en) 2006-12-28 2014-12-30 Cymabay Therapeutics, Inc. Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
US8975258B2 (en) 2006-12-28 2015-03-10 Cymabay Therapeutics, Inc. Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
US9150567B2 (en) 2009-10-01 2015-10-06 Cymabay Therapeutics, Inc. Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts

Also Published As

Publication number Publication date
EP1735622A2 (fr) 2006-12-27
WO2005116653A2 (fr) 2005-12-08
JP5769361B2 (ja) 2015-08-26
JP2008263979A (ja) 2008-11-06
JP2007532135A (ja) 2007-11-15
US20080306114A1 (en) 2008-12-11
CN101027560A (zh) 2007-08-29
TW200539867A (en) 2005-12-16
JP2015064359A (ja) 2015-04-09
CA2564139A1 (fr) 2005-12-08
AU2005248722A1 (en) 2005-12-08
JP2012050454A (ja) 2012-03-15

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